Биологическая активность
CCR2 covalent-IN-14 is a covalent, negative allosteric modulator (NAM) of CCR2, binds to intracellularly pocket of CCR2 with Ki of 4 nM.CCR2 covalent-IN-14 is more мощный than non-covalent analogue and wash-resistant in functional assays (IC50=33 nM in GTPγS связывание assay on U2OS-CCR2 клетка membranes, IC50=4 nM in β-arrestin recruitment assays).CCR2 covalent-IN-14 displays little to no inhibitory potency on CCR1 and CCR5.The affinity of CCR2 covalent-IN-14 for both the C70S and C75S CCR2 mutants is significantly decreased compared to WT CCR2.
Оригинал на английском
CCR2 covalent-IN-14 is a covalent, negative allosteric modulator (NAM) of CCR2, binds to intracellularly pocket of CCR2 with Ki of 4 nM.CCR2 covalent-IN-14 is more potent than non-covalent analogue and wash-resistant in functional assays (IC50=33 nM in GTPγS binding assay on U2OS-CCR2 cell membranes, IC50=4 nM in β-arrestin recruitment assays).CCR2 covalent-IN-14 displays little to no inhibitory potency on CCR1 and CCR5.The affinity of CCR2 covalent-IN-14 for both the C70S and C75S CCR2 mutants is significantly decreased compared to WT CCR2.
Химические свойства
- CAS №
- 2714478-83-6
- Брутто-формула
- C₂₃H₁₆Cl₂F₃N₃O₄S₂
- Мол. масса
- 590.41 г/моль
Хранение и физические свойства
- Условия хранения
- 2 года -20°C порошок, 2 недели 4°C в ДМСО, 6 мес. -80°C в ДМСО
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.